Beta 1 adrenergic blocker

Active ingredient

Release form, composition and packaging

Pills white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel ("double step" shape) on one side and an engraving "E435" on the other side, odorless.

Excipients: microcrystalline cellulose - 41.5 mg, sodium carboxymethyl starch (type A) - 7.5 mg, colloidal anhydrous silicon dioxide - 2 mg, K90 - 2 mg, magnesium stearate - 2 mg.

20 pcs. - blisters (3) - cardboard packs.

Pills white or almost white, round, biconvex, with a mark on one side and an engraving “E434” on the other side, odorless.

Excipients: microcrystalline cellulose - 83 mg, sodium carboxymethyl starch (type A) - 15 mg, colloidal anhydrous silicon dioxide - 4 mg, povidone K90 - 4 mg, magnesium stearate - 8 mg.

15 pcs. - blisters (4) - cardboard packs.
60 pcs. - dark glass jars (1) - cardboard packs.

Pills white or almost white, round, biconvex, chamfered, with a mark on one side and engraved “E432” on the other side, odorless.

Excipients: microcrystalline cellulose - 166 mg, sodium carboxymethyl starch (type A) - 30 mg, colloidal anhydrous silicon dioxide - 8 mg, povidone K90 - 8 mg, magnesium stearate - 8 mg.

30 pcs. - dark glass jars (1) - cardboard packs.
60 pcs. - dark glass jars (1) - cardboard packs.

Pharmacological action

Cardioselective β-adrenergic receptor blocker.

Metoprolol suppresses the effects increased activity sympathetic system on the heart, and also causes rapid decline Heart rate, contractility, output and blood pressure.

At arterial hypertension metoprolol reduces blood pressure in patients standing and lying down. The long-term antihypertensive effect of the drug is associated with a gradual decrease in peripheral vascular resistance. For arterial hypertension long-term use The drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function. In men with mild or moderate degree hypertension, metoprolol reduces mortality from cardiovascular causes(first of all, sudden death, fatal and non-fatal heart attack and stroke).

— functional disorders cardiac activity accompanied by tachycardia;

— IHD (secondary prevention of myocardial infarction, prevention of angina attacks);

- heart rhythm disturbances (supraventricular arrhythmias, ventricular extrasystole);

- hyperthyroidism (as part of complex therapy);

- prevention of migraine attacks.

Contraindications

— cardiogenic shock;

- AV block II and III degree;

- sinoatrial block;

— sinus bradycardia(heart rate<50 уд./мин);

— heart failure in the stage of decompensation;

- severe peripheral circulatory disorders;

- age under 18 years (due to the lack of sufficient clinical data);

- simultaneous intravenous administration of verapamil;

- severe form of bronchial asthma;

- pheochromocytoma without simultaneous use of alpha-blockers;

- hypersensitivity to metoprolol or any other component of the drug;

- increased sensitivity to other beta-blockers.

Due to insufficient clinical data, Egiolok is contraindicated in acute myocardial infarction accompanied by heart rate<45 уд./мин, с интервалом PQ >240 ms, and systolic blood pressure<100 мм рт.ст.

With caution the drug should be prescribed for diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal/liver failure; myasthenia gravis; pheochromocytoma (when used simultaneously with alpha-blockers); thyrotoxicosis; AV blockade of the first degree, depression (including a history); psoriasis; obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; during lactation; elderly patients; patients with a history of allergic reactions (possible decreased response when using adrenaline).

Dosage

The drug should be taken orally during or regardless of meals. If necessary, the tablet can be broken in half.

The dose should be adjusted gradually and individually to avoid the development of excessive bradycardia. The maximum daily dose is 200 mg.

At mild or moderate arterial hypertension The initial dose is 25-50 mg 2 times a day (morning and evening). If necessary, the dose can be gradually increased to 100-200 mg/day or another antihypertensive agent can be added.

At angina pectoris the initial dose is 25-50 mg 2-3 times/day. Depending on the effect, the dose can be gradually increased to 200 mg/day or another antianginal drug can be added.

At heart rhythm disturbances the initial dose is 25-50 mg 2-3 times/day. If necessary, the daily dose can be gradually increased to 200 mg/day or another antiarrhythmic agent can be added.

At hyperthyroidism the usual daily dose is 150-200 mg in 3-4 doses.

At functional heart disorders accompanied by palpitations the usual dose is 50 mg 2 times / day (morning and evening); if necessary, the dose can be increased to 200 mg in 2 doses.

For prevention of migraine attacks The recommended dose is 100 mg/day in 2 divided doses (morning and evening); if necessary, the dose can be increased to 200 mg/day in 2 divided doses.

U patients with renal dysfunction no change in dosage regimen is required.

In liver cirrhosis, dose changes are usually not required due to the low binding of metoprolol to plasma proteins. At severe liver failure(for example, after portacaval shunting), it may be necessary to reduce the dose of Egilok.

U elderly patients no dose adjustment is required.

Side effects

Egilok is usually well tolerated by patients. Side effects are usually mild and reversible. The following side effects have been reported in clinical trials and during therapeutic use of metoprolol. In some cases, the connection between an adverse event and the use of the drug has not been reliably established. The frequency of side effects listed below is defined as follows: very common (>10%), common (1-9.9%), uncommon (0.1-0.9%), rare (0.01-0.09%), very rare, including isolated reports (<0.01%).

From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - increased excitability, anxiety; uncommon - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; very rarely - amnesia/memory impairment, depression, hallucinations.

From the cardiovascular system: often - bradycardia, orthostatic hypotension (in some cases, syncope is possible), coldness of the lower extremities, palpitations; uncommon - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV block of the first degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).

From the respiratory system: often - shortness of breath during physical effort; uncommon - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.

From the skin: uncommon - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis.

From the senses: rarely - blurred vision, dryness and/or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, disturbance of taste.

From the reproductive system: rarely - impotence/sexual dysfunction.

Others: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia.

The use of Egilok should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably determined.

Overdose

Symptoms: marked decrease in blood pressure, sinus bradycardia, AV block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase when used simultaneously with ethanol, antihypertensive drugs, quinidine and barbiturates.

The first symptoms of overdose appear 20 minutes to 2 hours after taking the drug.

Treatment: Careful monitoring of the patient is necessary (monitoring blood pressure, heart rate, respiratory rate, renal function, blood glucose concentration, serum electrolytes) in the intensive care unit. If the drug has been taken recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if lavage is not possible, vomiting may be induced if the patient is conscious). In case of excessive decrease in blood pressure, bradycardia and threat of heart failure - intravenous administration of beta-adrenergic agonists (until the desired effect is achieved) or intravenous administration of 0.5-2 mg of atropine at intervals of 2-5 minutes. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). For hypoglycemia - administration of 1-10 mg of glucagon, installation of a temporary pacemaker. For bronchospasm - administration of beta 2-adrenergic agonists. For convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

Drug interactions

The antihypertensive effects of Egilok are usually enhanced when used concomitantly with other antihypertensive drugs. To avoid hypotension, careful monitoring of patients receiving combinations of these drugs is necessary. However, the summation of the effects of antihypertensive drugs can be used, if necessary, to achieve effective blood pressure control.

The simultaneous use of metoprolol and slow calcium channel blockers such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. IV administration of the verapamil type should be avoided in patients receiving beta-blockers.

Combinations requiring caution

Oral antiarrhythmic drugs (such as quinidine and amiodarone): risk of bradycardia, AV block.

Cardiac glycosides: risk of developing bradycardia, conduction disorders; metoprolol does not affect the positive inotropic effect of cardiac glycosides.

Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups): risk of developing arterial hypotension and/or bradycardia.

Discontinuation of the simultaneous use of metoprolol and clonidine should be started by discontinuing metoprolol, and then (after a few days) clonidine; If clonidine is first discontinued, a hypertensive crisis may develop.

Some drugs acting on the central nervous system (for example, hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol): risk of developing arterial hypotension.

Anesthesia: risk of cardiac depression.

Alpha and beta sympathomimetics: risk of developing arterial hypertension, significant bradycardia, possible cardiac arrest.

Ergotamine: increased vasoconstrictor effect.

Beta 2 sympathomimetics: functional antagonism.

NSAIDs (for example, indomethacin): the antihypertensive effect may be weakened.

Estrogens: the antihypertensive effect of metoprolol may be reduced.

Oral hypoglycemic agents and insulin: Metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia.

Curare-like muscle relaxants: increased neuromuscular blockade.

Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline): the effects of metoprolol may be enhanced due to an increase in its concentration in the blood plasma.

Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism.

Concomitant use of sympathetic ganglion blockers or other beta blockers (eg, eye drops) or MAO inhibitors requires careful medical monitoring.

Special instructions

When prescribing Egilok, heart rate and blood pressure should be regularly monitored. The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation in case of heart rate<50 уд./мин.

In patients with diabetes mellitus, blood glucose levels should be regularly monitored and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

When using the drug at a dose exceeding 200 mg/day, cardioselectivity decreases.

Prescribing Egilok to patients with chronic heart failure is possible only after reaching the compensation stage.

In patients taking Egilok, the severity of hypersensitivity reactions may increase (against the background of a burdened allergic history) and there may be no effect from the administration of usual doses of epinephrine (adrenaline).

Anaphylactic shock may be more severe in patients taking Egilok.

The use of Egilok may worsen the symptoms of peripheral circulatory disorders.

Egilok should be discontinued gradually, gradually reducing its dose over 14 days. Abrupt cessation of treatment may increase angina attacks and the risk of developing coronary disorders. During drug withdrawal, patients with coronary artery disease should be under close medical supervision.

For exertional angina, the selected dose of Egilok should ensure the heart rate at rest is within 55-60 beats/min, and during exercise - no more than 110 beats/min.

Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid.

Egilok may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.

In diabetes mellitus, taking Egilok can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.

When prescribing metoprolol to patients with bronchial asthma, simultaneous use of beta 2-adrenergic agonists is necessary.

In patients with pheochromocytoma, Egilok should be used in combination with alpha-blockers.

Before performing any surgical intervention, it is necessary to inform the surgeon/anesthesiologist about the therapy being carried out with Egilok (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.

Drugs that reduce catecholamine levels (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.

When prescribing the drug to elderly patients, liver function should be regularly monitored. Correction of the dosage regimen is required only if increasing bradycardia appears in elderly patients (<50 уд./мин), выраженного снижения АД (систолическое АД <100 мм рт.ст.), AV-блокады, бронхоспазма, желудочковых аритмий, тяжелых нарушений функции печени. Иногда необходимо прекратить лечение.

In patients with severe renal failure, monitoring of renal function is recommended.

Special monitoring of the condition of patients with depressive disorders should be carried out. In case of development of depression caused by the use of beta-blockers, therapy should be discontinued.

If progressive bradycardia occurs, the dose should be reduced or the drug discontinued.

Use in pediatrics

Due to the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents under 18 years of age.

Impact on the ability to drive vehicles and operate machinery

Caution must be exercised when driving vehicles and when engaging in potentially hazardous activities that require increased concentration (risk of dizziness and fatigue).

Pregnancy and lactation

The use of the drug is not recommended during pregnancy. The use of the drug is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during pregnancy, careful monitoring of the condition of the fetus and newborn is necessary for 48-72 hours after birth, since bradycardia, arterial hypotension, hypoglycemia and respiratory depression may develop.

Despite the fact that when the drug is used in therapeutic doses, only a small amount of metoprolol is excreted in breast milk, the condition of the newborn should be monitored (bradycardia is possible). The use of the drug during lactation is not recommended. If it is necessary to use Egilok during lactation, breastfeeding should be stopped.

Severe liver failure

Latin name: Egilok S

ATX code: C07AB02

Active ingredient: metoprolol

Manufacturer: Intas Pharmaceuticals, Ltd. (Intas Pharmaceuticals, Ltd.) (India)

Updating the description and photo: 30.11.2018

Egilok S is a beta 1-adrenergic blocker with selective action.

Release form and composition

Dosage form – long-acting tablets, film-coated: biconvex, oval, white, with a score on both sides (10 pieces in a blister, in a cardboard pack of 3 or 10 blisters and instructions for use of Egilok S).

Composition of 1 tablet:

• active substance: metoprolol succinate – 25, 50, 100 or 200 mg;
• auxiliary components: ethylcellulose, methylcellulose, microcrystalline cellulose, glycerol, magnesium stearate, corn starch;
• film shell: Sepifilm LP 770 white (hypromellose, titanium dioxide E171, stearic acid, microcrystalline cellulose).

Pharmacological properties

Pharmacodynamics

The active substance of Egilok S, metoprolol succinate, is a beta 1-adrenergic blocker that is capable of blocking β 1 -adrenergic receptors when using significantly lower doses than those required to block β 2 -adrenergic receptors.

Egilok S has insignificant membrane-stabilizing activity and is not a partial agonist.

Metoprolol is able to reduce or suppress the agonistic effect exerted on cardiac activity by catecholamines, which are released during physical and nervous stress. This means that the drug can prevent an increase in cardiac output and heart rate (HR), increased cardiac contractility and an increase in blood pressure (BP) due to a sharp release of catecholamines.

Unlike conventional tablet selective beta 1 blockers (including metoprolol tartrate), extended-release metoprolol succinate provides a constant plasma concentration of the drug and a stable clinical effect (beta 1 blockade) for at least 24 hours. As a result of the absence of significant maximum plasma concentrations of metoprolol succinate has higher β 1 -selectivity than conventional tablet forms of metoprolol. In addition, Egilok S significantly reduces the potential risk of side effects that often occur at maximum plasma concentrations, such as weakness in the legs when walking or bradycardia.

For concomitant obstructive pulmonary diseases, Egilok S can be prescribed in addition to beta 2 adrenergic agonists. Metoprolol succinate has less effect on the bronchodilation they cause compared to non-selective beta-blockers.

Metoprolol succinate has less effect than non-selective beta-blockers on carbohydrate metabolism and insulin production, as well as on the cardiovascular system under conditions of hypoglycemia.

In case of arterial hypertension, Egilok S significantly reduces blood pressure, this effect persists for at least 24 hours, both in a lying and standing position, and during physical activity. At the beginning of drug use, an increase in vascular resistance is observed. However, with prolonged use of metoprolol succinate, a decrease in blood pressure is possible due to a decrease in vascular resistance, while cardiac output does not change.

Pharmacokinetics

Each Egilok S tablet contains a large number of microgranules (pellets) coated with a polymer shell, due to which a controlled release of the active substance is carried out.

The effect of the drug occurs quickly. Once in the gastrointestinal tract (GIT), the tablets are disintegrated into separate pellets, each of which acts separately, and together they provide a uniform release of metoprolol succinate for more than 20 hours. The rate of release depends on the acidity of the gastric environment. Thus, the duration of action of Egilok S is more than 24 hours.

Metoprolol succinate is completely absorbed from the gastrointestinal tract. After a single dose, systemic bioavailability is approximately 30–40%.

The substance is characterized by low binding to plasma proteins – 5–10%.

The drug is metabolized in the liver by oxidation to form three main metabolites that do not have clinically significant activity. It is excreted mainly in the form of metabolites, only about 5% of the dose is eliminated unchanged by the kidneys.

The half-life of free metoprolol is ~3.5–7 hours.

Indications for use

• stable chronic heart failure, accompanied by clinical manifestations (II–IV functional class according to the NYHA classification) and impaired left ventricular systolic function (as an additional drug as part of the main treatment of chronic heart failure);
• arterial hypertension;
• heart rhythm disturbances, including supraventricular tachycardia, decreased ventricular contraction frequency during ventricular extrasystoles and atrial fibrillation;
• angina pectoris;
• functional disorders of cardiac activity accompanied by tachycardia;
• reduction in the incidence of re-infarction and mortality after the acute phase of myocardial infarction;
• prevention of migraine attacks.

Contraindications

Absolute:

• arterial hypotension at systolic blood pressure< 90 мм рт. ст.;
• sick sinus syndrome (SSNS);
• atrioventricular block II and III degrees;
• clinically significant sinus bradycardia with heart rate< 50 уд/мин;
• decompensated heart failure;
• P-Q interval > 0.24 sec;
• suspicion of acute myocardial infarction at heart rate< 45 уд/мин;
• cardiogenic shock;
• severe peripheral circulatory disorders with the threat of gangrene;
• pheochromocytoma (if alpha-blockers are not used simultaneously);
• age under 18 years;
• intravenous (IV) administration of slow calcium channel blockers such as verapamil;
• simultaneous use of monoamine oxidase inhibitors (MAO) (except type B);
• long-term or course use of inotropic agents and drugs acting on β-adrenergic receptors;
• hypersensitivity to any component of the drug or other beta-blockers.

Egilok S tablets should be used with caution in the following cases (a careful assessment of the benefit-risk ratio is required):

• Prinzmetal's angina;
• atrioventricular block of the first degree;
• obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);
• metabolic acidosis;
• severe renal/liver failure;
• chronic obstructive pulmonary disease;
• bronchial asthma;
• diabetes mellitus;
• thyrotoxicosis;
• psoriasis;
• myasthenia gravis;
• depression;
• pheochromocytoma (with simultaneous use of alpha-blockers);
• simultaneous use of cardiac glycosides;
• old age.

Egilok S, instructions for use: method and dosage

Egilok S is taken orally, 1 time per day (regardless of the prescribed dose), preferably in the morning. The tablets must be swallowed whole, without chewing or crumbling, and washed down with a sufficient amount of liquid. Meal times don't matter.

The optimal dose is selected individually by the doctor, with caution to avoid the development of bradycardia.

Treatment of stable chronic heart failure (CHF) with clinical manifestations and impaired left ventricular systolic function begins only if the patient is in a stable condition without episodes of exacerbation during the last 6 weeks. However, during the last 2 weeks the main therapy regimen cannot be changed.

In some cases, beta-blockers (including Egilok S) can cause a temporary worsening of chronic heart failure. Sometimes it is possible to extend therapy or reduce the dose, but some patients require discontinuation of metoprolol.

For functional class II CHF, 25 mg is prescribed at the beginning of therapy; after 2 weeks, if necessary, the dose is increased to 50 mg. If in this case the effect is not enough, further doubling of the dose is possible at intervals of 2 weeks. For long-term treatment, the maintenance dose is usually 200 mg.

For CHF of functional classes III and IV, Egilok S is prescribed in the first two weeks at a daily dose of 12.5 mg (½ tablet at a dosage of 25 mg). The optimal maintenance dose is selected individually under close medical supervision, since progression of heart failure symptoms is possible. After 1–2 weeks, if necessary, increase the daily dose to 25 mg, after another 2 weeks – to 50 mg. If the therapeutic effect is insufficient, but provided the drug is well tolerated, it is possible to double the dose at intervals of 2 weeks until the maximum is reached - 200 mg.

If arterial hypotension and/or bradycardia develops, it may be necessary to adjust the main therapy regimen or reduce the dose of Egilok S. The development of arterial hypotension during dose selection does not always indicate intolerance to the drug at this dose when treatment is continued. However, the dose can be further increased only after the patient’s condition has stabilized. Sometimes monitoring of the functional state of the kidneys is required.

• arterial hypertension: 50–100 mg. If the effect is insufficient, increase the daily dose to a maximum of 200 mg or add another antihypertensive drug to therapy (preference is given to diuretics and slow calcium channel blockers);
• heart rhythm disturbances: 100–200 mg;
• angina: 100–200 mg. If the therapeutic effect is insufficient, another antianginal agent is added to therapy;
• functional disorders of cardiac activity accompanied by tachycardia: 100 mg, if necessary, the daily dose is increased to 200 mg;
• maintenance therapy after myocardial infarction: 100–200 mg (in this case, the daily dose can be divided into 2 doses);
• prevention of migraine attacks: 100–200 mg.

Elderly persons, patients with impaired renal function and patients with moderate impairment of liver function do not need to adjust the dose.

In case of severe functional disorders of the liver (severe cirrhosis, portocaval anastomosis), it may be necessary to reduce the dose of Egilok S.

Side effects

Egilok S is generally well tolerated. If adverse reactions occur, they are usually mild and reversible.

Possible side effects (classified as follows: very often - > 10% of cases; often - 1-9.9%; infrequently - 0.1-0.9%; rarely - 0.01-0.09%; very rarely -< 0,01%):

• from the cardiovascular system: often - palpitations, orthostatic hypotension (very rarely accompanied by fainting), bradycardia, cold extremities; uncommon - temporary increase in symptoms of heart failure, pain in the heart area, peripheral edema, first degree atrioventricular block, cardiogenic shock in patients with acute myocardial infarction; rarely - other cardiac conduction disorders, arrhythmias; very rarely in patients with previous severe peripheral circulatory disorders - gangrene;
• from the digestive system: often – abdominal pain, constipation, diarrhea, nausea; infrequently - vomiting; rarely – dryness of the oral mucosa, functional liver disorder; very rarely - hepatitis;
• from the central nervous system: very often – increased fatigue; often – headache, dizziness; uncommon – insomnia/drowsiness, nightmares, loss of attention, paresthesia, depression, convulsions; rarely - anxiety, increased nervous excitability, sexual dysfunction/impotence; very rarely - depression, memory impairment/amnesia, hallucinations;
• from the senses: rarely - dryness and/or irritation of the eyes, visual disturbances, conjunctivitis; very rarely - taste disturbances, ringing in the ears;
• from the respiratory system: often – shortness of breath with physical effort; uncommon – bronchospasm; rarely – rhinitis;
• from the musculoskeletal system: very rarely - arthralgia;
• from the skin: infrequently – urticaria, increased sweating; rarely – hair loss; very rarely - exacerbation of psoriasis, photosensitivity;
• other: infrequently - weight gain; very rarely - thrombocytopenia.

Overdose

The most serious symptoms of metoprolol succinate overdose are disorders of the cardiovascular system, but sometimes suppression of pulmonary function and predominance of symptoms from the central nervous system are possible.

Possible symptoms: marked decrease in blood pressure, AV block I–III degree, bradycardia, weak peripheral perfusion, asystole, cardiogenic shock, heart failure, apnea, depression of pulmonary function, bronchospasm, impairment or loss of consciousness, increased fatigue, increased sweating, tremor, paresthesia, convulsions, esophageal spasm, nausea, vomiting, renal dysfunction, hyperkalemia, hyperglycemia, hypoglycemia (especially in children), transient myasthenic syndrome. Concomitant use of alcohol, barbiturates, antihypertensive drugs or quinidine may worsen the patient's condition. The first symptoms of overdose may occur 20–120 minutes after taking high doses of Egilok S.

First aid measures: taking activated carbon, and, if necessary, gastric lavage. Before gastric lavage, due to the risk of stimulating the vagus nerve, atropine is prescribed (adults - 0.25–0.5 mg). If required, ensure airway patency (by intubation) and adequate ventilation. It is necessary to administer glucose, replenish the volume of circulating blood, and monitor the electrocardiogram. Atropine is also administered at a dose of 1–2 mg intravenously; the administration is repeated as necessary (especially in the presence of vagal symptoms). For depression (suppression) of the myocardium, an infusion of dopamine or dobutamine is given. In addition, it is possible to administer glucagon intravenously at 50–150 mcg/kg at intervals of 1 minute. In some cases, it is advisable to add epinephrine (adrenaline) to therapy. For arrhythmia and dilated ventricular complex, infusion of 0.9% sodium chloride solution or sodium bicarbonate is indicated. If necessary, an artificial pacemaker is installed. To relieve bronchospasm, terbutaline is used (injection or inhalation). In case of cardiac arrest, appropriate resuscitation measures are carried out.

Special instructions

Beta blockers are not recommended for patients with obstructive pulmonary disease. If other antihypertensive drugs are poorly tolerated or do not have the desired therapeutic effect, Egilok S can be used, but the minimum effective dose should be prescribed. If necessary, use beta 2-adrenergic agonists.

Compared to non-selective beta-blockers, selective beta 1-blockers have a lesser effect on carbohydrate metabolism and mask the symptoms of hypoglycemia, but the risk of such an effect cannot be completely excluded.

In case of decompensated chronic heart failure, the stage of compensation should be achieved before starting treatment, and it should be maintained during therapy.

Data from clinical studies on the safety and effectiveness of Egilok S in severe stable heart failure (NYHA class IV) are limited.

Metoprolol succinate may worsen symptoms of peripheral circulatory disorders (usually due to a decrease in blood pressure).

For patients with concomitant pheochromocytoma, Egilok S is prescribed simultaneously with an alpha-blocker.

In rare cases, if atrioventricular conduction is impaired, it may worsen (even to AV block). If bradycardia develops, the dose of metoprolol succinate should be reduced or gradually discontinued.

Patients undergoing surgery should warn the anesthesiologist about taking Egilok S. It is not recommended to discontinue beta-blockers.

Anaphylactic shock that develops during therapy with beta-blockers occurs in a more severe form. However, the use of adrenaline in standard therapeutic doses does not always produce the desired effect.

The effectiveness and safety of Egilok S in patients with symptoms of heart failure in combination with acute myocardial infarction and unstable angina have not been established.

If the drug is abruptly discontinued, symptoms of chronic heart failure may increase, and the risk of myocardial infarction and sudden death may increase, especially in high-risk patients. For this reason, it is not recommended to suddenly stop taking Egilok S. This should be done gradually, over a minimum of 2 weeks, reducing the dose by half at each stage, until the final dose of 12.5 mg is reached - it should be taken for at least 4 days until the drug is completely discontinued. If undesirable symptoms appear with this regimen, a slower withdrawal of therapy is recommended.

Impact on the ability to drive vehicles and complex mechanisms

Egilok S can cause dizziness and increased fatigue, so patients receiving the drug should be careful when driving vehicles and performing potentially hazardous types of work.

Use during pregnancy and lactation

Adequate controlled studies on the use of metoprolol succinate in pregnant women have not been conducted. As a result, Egilok S can only be used in women for whom the expected benefits of therapy outweigh the possible risks.

Beta blockers may cause some side effects in fetuses, newborns, and infants, such as bradycardia.

Metoprolol passes into mother's milk in small quantities, so the risk of adverse reactions is low. However, infants whose mothers receive Egilok S during lactation should be under close medical supervision for possible signs of β-adrenergic receptor blockade.

Use in childhood

Egilok S is contraindicated under 18 years of age, since its effectiveness and safety in pediatric patients have not been established.

For impaired renal function

For patients with chronic renal failure, Egilok S is prescribed with caution.

Correction of the dosage regimen for functional renal impairment and hemodialysis is not required.

For liver dysfunction

For patients with liver failure, Egilok S is prescribed with caution. The doctor selects the dose individually, based on the clinical condition.

Use in old age

For the treatment of elderly patients, Egilok S tablets are used with precautions.

Drug interactions

• verapamil: high risk of developing bradycardia and lowering blood pressure, there is a complementary inhibitory effect on AV conduction and sinus node function;
• barbituric acid derivatives: increases the metabolism of metoprolol;
• propafenone: plasma concentration of metoprolol increases significantly (2–5 times), side effects may develop.

Combinations that require caution and may require dose adjustment:

• Class I antiarrhythmic drugs: the negative inotropic effect may be additive, which can lead to the development of serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with AV conduction defects and sick sinus syndrome;
• non-steroidal anti-inflammatory drugs (with the possible exception of sulindac): the antihypertensive effect of metoprolol is weakened;
• cardiac glycosides: AV conduction time increases, bradycardia develops;
• clonidine: after its abrupt withdrawal, hypertensive reactions may increase (it is recommended to start stopping beta-blockers several days before stopping the use of clonidine);
• quinidine: in patients with rapid hydroxylation, the metabolism of metoprolol is inhibited, which causes a significant increase in its plasma concentration and increased beta-blockade (similar reactions are possible when using other beta-blockers, the metabolism of which involves the CYP2D6 isoenzyme);
• Rifampicin: it is possible to increase the metabolism of metoprolol and reduce its plasma concentration;
• oral hypoglycemic agents: there is a possibility of a change in their effect, which may require dose adjustment;
• inhalation anesthetics: increased cardiodepressive effect;
• Amiodarone: severe sinus bradycardia may develop. Amiodarone has a long half-life, so interactions may occur long after discontinuation;
• epinephrine: there is a risk of bradycardia and severe arterial hypertension;
• diltiazem: there is a mutual enhancement of the inhibitory effect on the conductivity and function of the sinus node, there are known cases of the development of severe bradycardia;
• phenylpropanolamine (norephedrine): it is possible to increase diastolic blood pressure to pathological values ​​and develop a hypertensive crisis (even after using a single dose of 50 mg);

Dispensed by prescription.

Catad_pgroup Beta blockers

Egilok tablets - official* instructions for use

*registered by the Ministry of Health of the Russian Federation (according to grls.rosminzdrav.ru)

Registration number: P No. 015639/01 03/17/2009

Trade name: Egilok ®

International nonproprietary name: metoprolol

Dosage form: pills

Compound: Each tablet contains 25 mg, 50 mg or 100 mg of the active substance metoprolol tartrate. Excipients: microcrystalline cellulose 41.5/83/166 mg, sodium carboxymethyl starch (type A) 7.5/15/30 mg, colloidal anhydrous silicon dioxide 2/4/8 mg, povidone (K-90) 2/4/ 8 mg, magnesium stearate 2/4/8 mg.

Description: 25 mg tablets: White or off-white, round, biconvex tablets with a cross-shaped dividing line and a double bevel (double snap shape) on one side and engraved E 435 on the other side, odorless.

Tablets 50 mg: White or almost white, round, biconvex tablets, scored on one side and engraved E 434 on the other side, odorless.

Tablets 100 mg: White or almost white, round, biconvex tablets, beveled, scored on one side and engraved E 432 on the other side, odorless.

Pharmacotherapeutic group: selective beta1-blocker

ATX code:С07АВ02

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics:

Mechanism of action:

Metoprolol suppresses the effects of increased sympathetic system activity on the heart and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.

At arterial hypertension metoprolol reduces blood pressure in patients in the standing and lying position. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function. In men with mild or moderate hypertension, metoprolol reduces mortality from cardiovascular causes (primarily sudden death, fatal and non-fatal heart attack and stroke).

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic blood pressure, heart rate and myocardial contractility. A decrease in heart rate and a corresponding prolongation of diastole when taking metoprolol ensures improved blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, for angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia, and improves the patient’s physical performance. In myocardial infarction, metoprolol reduces the mortality rate by reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A reduction in mortality can also be observed with the use of metoprolol in both the early and late phases of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus. Use of the drug after myocardial infarction reduces the likelihood of non-fatal recurrent infarction. In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken starting from low doses (2x5 mg/day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.

In case of supraventricular tachycardia, atrial fibrillation and ventricular extrasystoles, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles.

At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers.

Compared with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. It does not increase the duration of hypoglycemic attacks.

Metoprolol causes a slight increase in triglyceride concentrations and a slight decrease in serum free fatty acid concentrations. There is a significant decrease in total serum cholesterol concentrations after several years of taking metoprolol.

Pharmacokinetics:

Metoprolol is quickly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. The maximum concentration in blood plasma is achieved 1.5-2 hours after oral administration. After absorption, metoprolol undergoes significant first-pass metabolism through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with regular use.

Taking with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol is slightly (~ 5-10%) bound to plasma proteins. The volume of distribution is 5.6 l/kg.

Metoprolol is metabolized in the liver by cytochrome P-450 isoenzymes. Metabolites do not have pharmacological activity.

Half-life (t 1/2) on average 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l/min.

Approximately 95% of the administered dose is excreted by the kidneys, 5% as unchanged metoprolol. In some cases this value can reach 30%.

There were no significant changes in the pharmacokinetics of metoprolol in elderly patients.

Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases there is a decrease in the excretion of metabolites. In severe renal failure (glomerular filtration rate less than 5 ml/min), a significant accumulation of metabolites is observed. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade.

Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after a portacaval shunt, bioavailability may increase and overall body clearance may decrease. After portacaval shunt, the total clearance of the drug from the body is approximately 0.3 L/min, and the area under the concentration-time curve increases approximately 6 times compared with that in healthy volunteers.

INDICATIONS FOR USE

Arterial hypertension (in monotherapy or (if necessary) in combination with other antihypertensive drugs); functional disorders of cardiac activity, accompanied by tachycardia.

Coronary heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks.

Heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole). Hyperthyroidism (complex therapy). Prevention of migraine attacks.

CONTRAINDICATIONS

Hypersensitivity to metoprolol or any other component of the drug, as well as other beta-blockers; atrioventricular block (AV) II or III degree; sinoatrial block; sinus bradycardia (heart rate less than 50/min), sick sinus syndrome; cardiogenic shock; severe peripheral circulatory disorders; heart failure in the stage of decompensation, age under 18 years (due to the lack of sufficient clinical data), simultaneous intravenous administration of verapamil, severe bronchial asthma and pheochromocytoma without simultaneous use of alpha-blockers.

Due to insufficient clinical data, Egiolok ® is contraindicated in acute myocardial infarction, accompanied by a heart rate below 45 beats/min, with a PQ interval of more than 240 ms, and systolic blood pressure below 100 mm Hg.

WITH CAUTION

Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (COPD), renal/liver failure, myasthenia gravis, pheochromocytoma (with simultaneous use with alpha-blockers), thyrotoxicosis, AV block of the first degree, depression (including history), psoriasis, obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome), pregnancy, lactation, old age, in patients with a burdened allergic history (a decrease in response is possible when using adrenaline).

USE IN PREGNANCY AND LACTATION

The use of the drug is not recommended during pregnancy. The use of the drug is possible only when the benefit to the mother outweighs the potential risk to the fetus. If taking the drug is necessary, you should carefully monitor the fetus and then the newborn for several days (48 - 72 hours) after birth, as bradycardia, respiratory depression, decreased blood pressure and hypoglycemia may develop.

Although only small amounts of the drug are excreted into breast milk when taking therapeutic doses of metoprolol, the newborn should be kept under observation (bradycardia is possible). The use of the drug during lactation is not recommended. If it is necessary to use the drug during lactation, it is recommended to stop breastfeeding.

METHOD OF APPLICATION AND DOSES

Egilok ® tablets are taken orally. The tablets can be taken with food or without regard to meals. If necessary, the tablet can be broken in half. The dose should be adjusted gradually and individually to avoid excessive bradycardia. The maximum daily dose is 200 mg. Recommended doses:

Arterial hypertension

For mild or moderate arterial hypertension, the initial dose is 25-50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 100-200 mg/day or another antihypertensive agent can be added.

Angina pectoris

The initial dose is 25-50 mg two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day or another antianginal drug can be added.

Maintenance therapy after myocardial infarction

The usual daily dose is 100 - 200 mg/day, divided into two doses (morning and evening).

Heart rhythm disturbances

Initial dose is 25 to 50 mg two or three times daily. If necessary, the daily dose can be gradually increased to 200 mg/day or another antiarrhythmic agent can be added. Hyperthyroidism

The usual daily dose is 150-200 mg per day in 3 to 4 doses.

Functional heart disorders accompanied by palpitations The usual daily dose is 50 mg 2 times a day (morning and evening); if necessary, it can be increased to 200 mg in two doses.

Preventing migraine attacks

The usual daily dose is 100 mg/day in two divided doses (morning and evening); if necessary, it can be increased to 200 mg/day in 2 divided doses.

Special patient groups

If renal function is impaired, no change in dosage regimen is required.

In liver cirrhosis, a dose change is usually not required due to the low binding of metoprolol to plasma proteins (5-10%). In case of severe liver failure (for example, after portacaval shunt surgery), it may be necessary to reduce the dose of Egilok ®.

In elderly patients, no dose adjustment is required.

SIDE EFFECTS

Egilok ® is usually well tolerated by patients. Side effects are usually mild and reversible. The following side effects have been reported in clinical trials and during therapeutic use of metoprolol. In some cases, the connection between an adverse event and the use of the drug has not been reliably established. The frequency of side effects listed below is defined as follows: very common: > 10%), common: 1-9.9%, uncommon: 0.1-0.9%, rare: 0.01-0.09%, very rarely (including isolated messages):< 0,01 %.

From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - increased excitability, anxiety, impotence/sexual dysfunction; uncommon - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; very rarely - amnesia/memory impairment, depression, hallucinations.

From the cardiovascular system: often - bradycardia, orthostatic hypotension (in some cases, syncope is possible), coldness of the lower extremities, palpitations; uncommon - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, first degree atrioventricular block; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders). From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.

From the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis. From the respiratory system: often - shortness of breath with physical effort; uncommon - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

From the senses: rarely - blurred vision, dryness and/or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, disturbance of taste. Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia. Taking Egilok ® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably determined.

OVERDOSE

Symptoms: marked decrease in blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may be exacerbated by concomitant use of ethanol, antihypertensive drugs, quinidine and barbiturates.
The first symptoms of overdose appear 20 minutes -2 hours after taking the drug.

Treatment: Careful monitoring of the patient is necessary (monitoring blood pressure, heart rate, respiratory rate, renal function, blood glucose concentration, serum electrolytes) in the intensive care unit. If the drug has been taken recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if lavage is not possible, vomiting can be induced if the patient is conscious).

In case of excessive decrease in blood pressure, bradycardia and the threat of heart failure - intravenously, at intervals of 2-5 minutes, beta-adrenergic agonists - until the desired effect is achieved or intravenously 0.5-2 mg of atropine. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). For hypoglycemia - administration of 1-10 mg of glucagon, installation of a temporary pacemaker. For bronchospasm, beta2-agonists should be administered. For convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

INTERACTIONS WITH OTHER MEDICINES

The antihypertensive effects of Egilok ® and other antihypertensive drugs are usually enhanced. To avoid hypotension, careful monitoring of patients receiving combinations of these drugs is necessary. However, the summation of the effects of antihypertensive drugs can be used, if necessary, to achieve effective blood pressure control.

The simultaneous use of metoprolol and blockers of “slow” calcium channels such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. Intravenous administration of calcium channel blockers such as verapamil should be avoided in patients receiving beta-blockers.

Caution should be exercised when taken concomitantly with the following drugs:

Oral antiarrhythmic drugs (such as quinidine and amiodarone) - risk of bradycardia, atrioventricular block.

Cardiac glycosides (risk of bradycardia, conduction disorders; metoprolol does not affect the positive inotropic effect of cardiac glycosides).

Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups) due to the risk of hypotension and/or bradycardia.

Discontinuation of concomitant use of metoprolol and clonidine should be started by stopping metoprolol and then (after a few days) clonidine; If clonidine is first discontinued, a hypertensive crisis may develop.

Some drugs acting on the central nervous system, such as hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol, increase the risk of arterial hypotension. Anesthesia (risk of cardiac depression).

Alpha and beta sympathomimetics (risk of arterial hypertension, significant bradycardia; possibility of cardiac arrest). Ergotamine (increased vasoconstrictor effect). Beta-2 sympathomimetics (functional antagonism).

Nonsteroidal anti-inflammatory drugs (for example, indomethacin) may weaken the antihypertensive effect.

Estrogens (possibly reducing the antihypertensive effect of metoprolol). Oral hypoglycemic agents and insulin (metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia). Curare-like muscle relaxants (increased neuromuscular blockade). Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline) - enhance the effects of metoprolol due to an increase in its concentration in the blood plasma. Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism.

Concomitant use of sympathetic ganglion blockers or other beta blockers (eg eye drops) or monoamine oxidase inhibitors requires careful medical monitoring.

SPECIAL INSTRUCTIONS

Monitoring of patients taking beta-blockers includes regular measurement of heart rate (HR) and blood pressure, blood glucose concentration in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents for oral administration should be selected individually. The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose above 200 mg per day, cardioselectivity decreases.

In case of heart failure, treatment with Egilok ® begins only after reaching the stage of compensation of cardiac function.

There may be an increase in the severity of hypersensitivity reactions and a lack of effect from the administration of usual doses of epinephrine (adrenaline) in patients with a burdened allergic history.

Anaphylactic shock may be more severe in patients taking Egilok ® . May increase symptoms of peripheral arterial circulation disorders. Abrupt discontinuation of Egilok ® should be avoided. The drug should be discontinued gradually by reducing doses over approximately 14 days. Abrupt withdrawal may worsen angina symptoms and increase the risk of coronary events. When discontinuing the drug, special attention should be paid to patients with coronary artery disease. For angina pectoris, the selected dose of Egilok ® should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min. Patients who use contact lenses should take into account that during treatment with beta-blockers, a decrease in the production of tear fluid may occur. Egilok may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated as it can increase symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. When prescribing Egilok ® to patients with diabetes mellitus, the concentration of blood glucose should be monitored and, if necessary, the dose of insulin or oral hypoglycemic agents should be adjusted (see section “Interaction with other drugs”).

If necessary, beta2-adrenergic stimulants are prescribed to patients with bronchial asthma; for pheochromocytoma - alpha-blockers.

If surgical intervention is necessary, it is necessary to warn the surgeon/anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect); discontinuation of the drug is not recommended. Drugs that reduce catecholamine levels (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.

In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver dysfunction , sometimes it is necessary to stop treatment. In patients with severe renal failure, monitoring of renal function is recommended.

Special monitoring should be carried out for the condition of patients with depressive disorders taking metoprolol; in case of development of depression caused by taking beta-blockers, it is recommended to discontinue therapy.

If progressive bradycardia occurs, the dose should be reduced or the drug discontinued.

Due to the lack of sufficient clinical data, the drug is not recommended for use in children.

Impact on the ability to drive vehicles and complex equipment.

Caution must be exercised when driving vehicles and when engaging in potentially hazardous activities that require increased concentration (risk of dizziness and fatigue).

RELEASE FORM

Tablets 25 mg: 60 tablets in a brown glass bottle with a PE cap with an accordion shock absorber, with first opening control. 1 bottle along with instructions for use is packed in a cardboard box. Or 20 tablets in a blister made of PVC/PVDC//al. foil. 3 blisters along with instructions for use are packed in a cardboard box.

Egilok - instructions for use, indications, composition, side effects, analogues and price

EGILOK

Pills white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel (“double step” shape) on one side and an engraving “E435” on the other side, odorless.

Excipients: microcrystalline cellulose – 41.5 mg, sodium carboxymethyl starch (type A) – 7.5 mg, colloidal anhydrous silicon dioxide – 2 mg, povidone K90 – 2 mg, magnesium stearate – 2 mg.

20 pcs. – blisters (3) – cardboard packs.

Pills white or almost white, round, biconvex, with a mark on one side and an engraving “E434” on the other side, odorless.

Excipients: microcrystalline cellulose – 83 mg, sodium carboxymethyl starch (type A) – 15 mg, colloidal anhydrous silicon dioxide – 4 mg, povidone K90 – 4 mg, magnesium stearate – 8 mg.

15 pcs. – blisters (4) – cardboard packs.
60 pcs. – dark glass jars (1) – cardboard packs.

Pills white or almost white, round, biconvex, chamfered, with a mark on one side and engraved “E432” on the other side, odorless.

Excipients: microcrystalline cellulose – 166 mg, sodium carboxymethyl starch (type A) – 30 mg, colloidal anhydrous silicon dioxide – 8 mg, povidone K90 – 8 mg, magnesium stearate – 8 mg.

30 pcs. – dark glass jars (1) – cardboard packs.
60 pcs. – dark glass jars (1) – cardboard packs.

Pharmacological action

Cardioselective β-adrenergic receptor blocker.

Metoprolol suppresses the effect of increased activity of the sympathetic system on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.

For arterial hypertension, metoprolol reduces blood pressure in patients in standing and lying positions. The long-term antihypertensive effect of the drug is associated with a gradual decrease in peripheral vascular resistance.

In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function.

In men with mild or moderate hypertension, metoprolol reduces mortality from cardiovascular causes (primarily sudden death, fatal and non-fatal heart attack and stroke).

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic blood pressure, heart rate and myocardial contractility. A decrease in heart rate and a corresponding prolongation of diastole when taking metoprolol ensures improved blood supply and oxygen uptake by the myocardium with impaired blood flow.

Therefore, for angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia, and improves the patient’s physical performance. In myocardial infarction, metoprolol reduces the mortality rate by reducing the risk of sudden death.

This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A reduction in mortality can also be observed with the use of metoprolol in both the early and late phases of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus.

Use of the drug after myocardial infarction reduces the likelihood of non-fatal recurrent infarction.

In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken in low doses (2x5 mg/day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.

In case of supraventricular tachycardia, atrial fibrillation and ventricular extrasystoles, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles.

At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers.

Compared with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism and does not increase the duration of hypoglycemia attacks.

Metoprolol causes a slight increase in the concentration of triglycerides and a slight decrease in the concentration of free fatty acids in the blood serum. There is a significant decrease in total serum cholesterol concentrations after using metoprolol for several years.

Pharmacokinetics

Suction

Metoprolol is quickly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. Cmax in blood plasma is achieved 1.5-2 hours after oral administration. Bioavailability is approximately 50% with a single dose and approximately 70% with regular use. Taking the drug simultaneously with food can increase bioavailability by 30-40%.

Distribution

Metoprolol is slightly (approximately 5-10%) bound to plasma proteins. Vd is 5.6 l/kg.

Metabolism

After absorption, metoprolol is largely subject to a first-pass effect through the liver. Metabolized in the liver by cytochrome P450 isoenzymes. Metabolites do not have pharmacological activity.

Removal

T1/2 averages 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l/min. Approximately 95% of the administered dose is excreted by the kidneys, 5% as unchanged metoprolol. In some cases this value can reach 30%.

Pharmacokinetics in special clinical situations

There were no significant changes in the pharmacokinetics of metoprolol in elderly patients.

Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases there is a decrease in the excretion of metabolites. In severe renal failure (GFR

Source: https://health.mail.ru/drug/egilok/

At what pressure do you drink Egilok: instructions for use (tablets 25 mg, 50 mg and 100 mg, retard)

In this medical article you can familiarize yourself with the drug Egilok. The instructions for use will explain at what pressure the tablets can be taken, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the forms of release of the drug and its composition.

In the article, doctors and consumers can only leave real reviews about Egilok, from which you can find out whether the medicine helped in the treatment of coronary artery disease and arterial hypertension in adults and children, for which it is also prescribed. The instructions list analogues of Egilok, prices of the drug in pharmacies, as well as its use during pregnancy.

A medicine for the treatment of pathologies of the cardiovascular system is Egilok. Instructions for use indicate that tablets 25 mg, 50 mg and 100 mg, retard, help reduce the ventricular heart rate during supraventricular tachycardia, ventricular extrasystole and atrial fibrillation.

Release form and composition

The drug is available in the following dosage forms:

1. Tablets 25 mg, 50 mg and 100 mg.
2. Extended-release film-coated tablets 50 mg and 100 mg (Retard).
3. Extended-release film-coated tablets 25 mg, 50 mg, 100 mg and 200 mg (Egilok S).

One tablet of Egilok (Retard) contains 25, 50, 100 mg of the active substance (metoprolol tartrate), respectively.

For one tablet of Egilok S, the active substance (metoprolol succinate) accounts for 23.75, 47.5, 95, 190 mg, respectively.

Pharmacological action

The instructions refer to Egilok as a beta1-adrenergic blocking agent. The main active ingredient is metoprolol. It has antianginal, antiarrhythmic, and blood pressure-lowering effects. By blocking beta1-adrenergic receptors, the drug reduces the stimulating effect of the sympathetic nervous system on the heart muscle, quickly reducing heart rate and blood pressure.

The hypotensive effect of the drug is long-lasting, since peripheral vascular resistance decreases gradually. Against the background of long-term use of Egilok with high blood pressure, the mass of the left ventricle significantly decreases, it relaxes better in the diastolic phase.

According to reviews, the drug is able to reduce mortality from cardiovascular pathology in males with a moderate increase in blood pressure. Like analogues, Egilok reduces the heart's need for oxygen due to a decrease in pressure and heart rate.

Due to this, diastole is extended - the time during which the heart rests, which improves its blood supply and absorption of oxygen from the blood. This action reduces the frequency of angina attacks, and against the background of asymptomatic episodes of ischemia, the patient’s physical condition and quality of life are significantly improved.

The use of Egilok reduces the ventricular heart rate in atrial fibrillation, ventricular extrasystole and supraventricular tachycardia.

Compared to non-selective beta-blockers of Egilok's analogues, it has less pronounced vascular and bronchi constricting properties, and it also has less effect on carbohydrate metabolism.

Taking the drug for several years significantly reduces blood cholesterol.

Indications for use

What does Egilok (Retard, S) help with? Tablets are prescribed if the patient has:

• angina pectoris;
• myocardial infarction;
• impaired functional cardiac activity;
• abnormal heart rhythm (supraventricular tachycardia and bradycardia with ventricular extrasystoles and atrial febrillation);
• high blood pressure;
• prophylactic prevention of migraine attacks.

Indications for the use of tablets also apply to people over 60 years of age.

Instructions for use (at what pressure does it help)

Egilok tablets should be taken orally during or immediately after a meal when the pressure is more than 140 to 90. They can be divided in half, but not chewed.

• For angina pectoris, supraventricular arrhythmias, for the prevention of migraine attacks, a dose of 100-200 mg per day is prescribed in 2 doses (morning and evening).
• For secondary prevention of myocardial infarction, an average daily dose of 200 mg is prescribed in 2 divided doses (morning and evening).
• For functional disorders of cardiac activity accompanied by tachycardia, a daily dose of 100 mg is prescribed in 2 divided doses (morning and evening).
• For arterial hypertension, a daily dose of 50-100 mg per day is prescribed in 1 or 2 doses (morning and evening). If the therapeutic effect is insufficient, a gradual increase in the daily dose to 100-200 mg is possible.

In elderly patients, patients with impaired renal function, and also if hemodialysis is necessary, no change in dosage regimen is required. In patients with severe liver dysfunction, the drug should be used in lower doses due to the slower metabolism of metoprolol.

Contraindications

The use of Egilok is unacceptable for:

• breastfeeding;
• angiospastic angina;
• persons under 18 years of age;
• cardiogenic shock;
• severe arterial hypotension;
• heart failure in the decompensation phase;
• SSSU;
• severe bradycardia;
• AV blockade of the second and third degree;
• hypersensitivity to metoprolol and other components of the Egilok drug, from which these tablets can cause side effects;
• sinoatrial block.

This medicine is prescribed with extreme caution for the following pathologies: metabolic acidosis, diabetes mellitus, bronchial asthma, obliterating peripheral vascular disease, chronic obstructive pulmonary disease, chronic renal failure, myasthenia gravis, psoriasis, depression, chronic liver failure and thyrotoxicosis.

Side effects

According to reviews given by doctors, Egilok is sometimes able to cause:

• stomach ache;
• headache, fatigue;
• decreased heart rate;
• allergic reactions;
• rhinitis, nausea;
• dizziness;
• shortness of breath, bronchospasm;
• diarrhea, vomiting;
• depression, insomnia;
• increased sweating.

Children, pregnancy and breastfeeding

The use of Egilok during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during this period, careful monitoring of the condition of the fetus and newborn is necessary for 48-72 hours after birth, since intrauterine growth retardation, bradycardia, arterial hypotension, respiratory depression, and hypoglycemia are possible.

The effect of metoprolol on a newborn during breastfeeding has not been studied, therefore women taking Egilok should stop breastfeeding. The drug should be prescribed with caution to children and adolescents under the age of 18 years.

Special instructions

Before starting therapy and during treatment, blood pressure and heart rate should be monitored. If the heart rate drops below 50 beats per minute, medical attention is required.

Patients with diabetes should regularly monitor their glucose levels and adjust their insulin dosage if necessary. Egilok should be discontinued gradually, reducing the dosage over two weeks to avoid withdrawal syndrome, coronary disorders and angina.

In patients using contact lenses, tear secretion may be reduced. It is recommended to exercise caution when driving vehicles and when engaging in potentially hazardous activities that require increased concentration.

Drug interactions

The list of prohibited drugs for simultaneous use with Egilok is wide. Therefore, you should be especially careful when combining this drug with third-party medications.

• When mixed with ethanol, the pumping effect on the central nervous system increases.
• When mixed with oral hypoglycemic drugs and insulin, the likelihood of hypoglycemia increases.
• When mixed with verapamil, it can cause cardiac arrest.
• When mixed with beta-blockers (estrogens, theophylline, indomethacin), the hypotensive property of metoprolol is reduced.

Analogues of the drug Egilok

Analogues are determined by structure:

1. Metocard.
2. Egilok Retard.
3. Betalok ZOK.
4. Corvitol 100.
5. Metoprolol succinate.
6. Betalok.
7. Vasocardin.
8. Emzok.
9. Corvitol 50.
10. Metoprolol.
11. Metozok.
12. Metoprolol tartrate.
13. Metolol.
14. Metokor Adifarm.

Concor or Egilok - which is better?

An exact answer can only be given through an individual examination. However, in general, Concor has slightly fewer side effects compared to its analogue, and its use at low heart rates is more acceptable. Egilok has a stronger medicinal effect compared to Concor.

Vacation conditions and price

The average cost of Egilok (25 mg tablets No. 60) in Moscow is 135 rubles. The price of a dosage of 100 mg is 130 rubles for 30 tablets, 50 mg is 145 rubles. for 30 pcs. Dispensed by prescription.

Source: https://instrukciya-po-primeneniyu.ru/egilok.html

Egilok: instructions for use, at what pressure?

Egilok is a drug from the beta1-blocker group, produces an antianginal (myocardial oxygen saturation), antiarrhythmic and hypotensive effect.

It reduces the heart's need for oxygen, increases endurance during ischemic heart disease, reduces the risk of angina attacks, and the risk of heart attack. The medicine is used in the complex treatment of coronary artery disease, arrhythmia, angina pectoris, heart failure, in the treatment of migraine and hyperthyroidism.

Egilok is prescribed for conditions caused by increased blood pressure and hypoxia (oxygen starvation) of cardiac tissue, which is due to its complex positive effect on the heart and hypotensive effect. Recommended for arrhythmia, migraine, high blood pressure, if there are no contraindications.

Release form and composition

Available in the form of white tablets for oral administration:

• Egilok regular action: round, biconvex tablets with a dosage of 25 mg - with a cross-shaped line on one side and the number “E 435” on the other;
• Egilok of regular action: with a dosage of 50,100 mg of risk - on the one hand and “E 434” and “E 432” - on the other;
• Egilok Retard of all dosages: oblong biconvex tablets, white coated, have a score on both sides.
• Egilok S all dosages: white, oval, biconvex tablets with a score on both sides.

The active substance is metoprolol tartrate. One capsule of Egilok and Egilok Retard contains 25, 50, 100 mg of active ingredient (metoprolol tartrate). The active ingredient in Engilok S is metoprolol succinate (25-200 mg). Excipients: microcrystalline cellulose, povidone, sodium carboxymethyl, starch, magnesium stearate, colloidal silicon dioxide (titanium), etc.

Store for 5 years at room temperature. Use as prescribed by a cardiologist.

Egilok has a normal effect, while Egilok S and Egilok Retard have a prolonged (extended) effect, which reduces the likelihood of side effects.

All varieties of the drug are produced by the pharmaceutical concern EGIS Pharmaceuticals PLC (Hungary).

There is another variety - a cheap analogue of Egilok S - Egilok SR, produced under license by the pharmaceutical plant Intas Pharmaceuticals Ltd (India).

All forms of the drug are considered the same; the active substance in them is different salts of metoprolol (tartrate and succinate), which break down in the body and release metoprolol. The only difference is in the speed of absorption and onset of effect, as well as in the composition of the excipients.

Cost of the drug: in Russia 125 rubles, in Kyiv – 57-90 UAH.

Pharmacological properties

The active substance of the drug blocks beta 1 adrenergic receptors of the heart, which reduces the frequency of heart contractions, the force of myocardial contractions and the volume of blood pushed into the aorta.

Egilok reduces blood pressure. With long-term use of Engilok, the risk of sudden death from stroke, heart attack, hypertensive crises, and cardiac pathologies is reduced. By improving the oxygen supply to the heart, the drug increases a person’s activity and reduces the risk of angina attacks.

Egilok and Egilok Retard are used if the patient has hyperthyroidism or hyperkinetic cardiac syndrome for complex treatment of the disease.

Egilok and Egilok S are prescribed to avoid supraventricular arrhythmia. These drugs are indicated for heart failure.

Egilok Retard is used in conjunction with diuretic (diuretic) drugs, cardiac glycosides and ACE inhibitors.

In case of disruption of the left cardiac ventricle (systolic phase) and heart failure, Egilok S is more effective. This form of the drug reduces the likelihood of death in the late stages of a heart attack, eliminates tachycardia and myocardial dysfunction.

Egilok prevents repeated attacks of angina pectoris, tachycardia, and repeated attacks after a heart attack. The medicine does not cure these heart diseases, but increases the patient’s endurance during physical and emotional stress, maintaining normal heart function.

By eliminating the symptoms of heart disease, it allows a person to lead a normal life.

The active component of Egilok, metaprolol, reduces the stimulating effect on the heart of the sympathetic nervous system, lowers heart rate and blood pressure.

Gradually reduces peripheral vascular resistance and gives a hypotensive effect. Due to a decrease in blood pressure and heart rate, the myocardium's need for oxygen decreases.

Thanks to this, the patient's condition improves, and angina attacks become less frequent.

Instructions for use

Study the instructions for use of Egilok: at what pressure it is prescribed, doses, features and contraindications of the drug.

Egilok tablets are taken regardless of meal time, preferably at the same time of day. The dose is selected individually, taking into account the patient’s indications, increasing gradually, but not more than 200 mg/day.

The medicine is prescribed for the following pathologies:

1. With high blood pressure.
2. Angina pectoris (pain behind the sternum - “angina pectoris”).
3. Migraine (pulsating headache in any area of ​​the head - occipital, temporal, frontal).
4. Tachycardia (increased heart rate - 90 and >).
5. Bradycardia (slow heart rate).
6. Functional disorders of the heart.
7. Atrial febrilation.
8. Myocardial infarction.

To protect yourself from the risk of harming your health when using a blood pressure medication, you must carefully read the instructions, familiarize yourself with the features of the drug (contraindications, side effects, compatibility with other drugs) and follow the doctor’s recommendations. Do not exceed the permissible dose, monitor changes in condition.

To reduce blood pressure, the initial dose is 25-50 mg in 2 doses (morning and evening). If there is no desired effect, the dose may be increased by the attending physician.

Treatment of angina pectoris involves 25-50 mg/day with a possible increase to 200 mg and the addition of a 2nd drug to obtain the desired result. It is necessary to ensure that the heart rate at rest and during exercise does not go beyond the limits: 55-60 – 110 beats/min.

After myocardial infarction, 100-200 mg/day is prescribed for maintenance therapy; for arrhythmia, 25-50 mg 2-3 times/day. If the effectiveness is insufficient, the dose is increased to 200 mg or a second drug against arrhythmia is added.

For migraine attacks, Egilok is prescribed 100 mg per day in 2 divided doses. In elderly patients and patients with liver or kidney pathology, the dose of the drug is not increased.

The maximum therapeutic effect occurs 1.5 hours after administration. About 95% of the drug is biotransformed (processed) by the liver, 5% is excreted from the body by the kidneys.

When treated with Egilok, it reduces the secretion of tear fluid and discomfort may occur in patients who use contact lenses. If surgery is to be performed during your appointment, you must inform the anesthesiologist about this so that he can select an adequate anesthesia.

Treatment should be completed gradually, reducing the dose (every 2 weeks). Abrupt withdrawal may worsen the patient's condition.

Contraindications

Having a wide range of indications, the drug has a number of contraindications. You can use it only after making sure that there are no contraindications.

It is dangerous for patients with a slow heartbeat (50-60 beats/min or less), sick sinus syndrome.

Use in cases of sinoatrial blockade and peripheral circulatory disorders is undesirable. Should not be taken by hypotensive patients (low blood pressure)

If the patient has contraindications, it is necessary to reduce the dose of the drug, monitor the body’s reaction to taking Egilok in small doses, or select another drug.

The drug should not be taken if:

• bradycardia;
• heart failure during decompensation;
• cardiogenic shock;
• during breastfeeding;
• hypersensitivity to the components of the drug;
• sinoatrial and atrioventricular block (2-3rd degree);
• arterial hypotension (pronounced decrease in blood pressure);
• angiospastic angina.

Side effects

Research, physician observations and patient reviews have made it possible to compile a list of possible side effects from various human organs and systems.

Side effects during treatment with Egilok:

Cardiovascular system:

• pain in the heart area;
• palpitations, arrhythmia;
• swelling of the extremities (Egilok Retard, Egilok S);
• increased signs of heart failure;
• cardiogenic shock in patients after a heart attack;
• bradycardia;
• orthostatic hypotension (a sharp drop in blood pressure when standing up);
• fainting;
• coldness in lower extremities.

Nervous system:

• dizziness and headache;
• anxiety;
• fatigue;
• depression;
• decreased concentration;
• excitability;
• convulsions;
• Paresthesia (impaired sensitivity, “pins and needles”).

• nausea, vomiting;
• abdominal pain;
• dry mouth;
• constipation or diarrhea;
• liver pathologies (stagnation of bile, yellowing of the skin, whites of the eyes, dark urine);
• increased bilirubin in the blood;
• hepatitis (Egilok C).

Respiratory organs:

• shortness of breath on exertion;
• rhinitis;
• bronchospasm;

Skin:

• excessive sweating;
• hives (blisters and itching);
• rash, itchy skin;
• photosensitivity (increased sensitivity of the skin to sunlight);
• exanthema (skin rash);
• redness of the skin.

Sense organs:

• visual impairment;
• taste disturbance;
• dryness, irritation of eyes;
• tinnitus;
• conjunctivitis (inflammation of the mucous membrane of the eyes).

In the initial stages of taking the medicine, you may feel tired.

These effects are temporary and mild. If any of the effects manifest themselves clearly and for a long time, you should stop taking the drug and consult a doctor.

Overdose

If the dose of the drug is mistakenly exceeded, dizziness and bradycardia, sometimes nausea and vomiting, may occur. Blood pressure may decrease. Sometimes, when the dose of Egilok is exceeded, a patient experiences arrhythmia, ventricular extrasystole, and may faint.

In severe cases of cardiogenic shock, the patient may lose consciousness and fall into a coma, and cardiac arrest may occur. With an excessive dose of the drug, such symptoms appear in the period from 20 minutes to 2 hours after administration.

If this happens, the patient needs to:

• rinse the stomach;
• give adsorbents;
• lay horizontally, raising your legs above your head (if the pressure has dropped);
• beta-adrenergic stimulants are administered intravenously (if bradycardia, heart failure has developed);
• Use Dopamine, Dobutamine, Norepinephrine if the measures taken do not help.

Doctors use different types of therapy, focusing on the patient's symptoms and condition. If this happens at home, you should immediately call an ambulance, explaining the essence of the problem.

Egilok's analogues

There are many analogues of the drug, but before using them you need to consult a cardiologist, but they cannot fully replace the original. Analogues: Vasocardin, Betalok, Corvitol, Lidalok, Metocard, Metozok, Metolol, Emzok, Metoprolol.

The simultaneous use of Egilok with certain drugs is prohibited:

• the hypotensive effect of metoprolol may be reduced with the combined use of Angilok and beta-blockers (theophylline, indomethacin, estrogens);
• when taken simultaneously with Verapamil, it can lead to cardiac arrest.
• simultaneous use with Ethanol will increase the negative effect on the central nervous system;
• the likelihood of hypoglycemia will increase when Egilok is mixed with insulin and hypoglycemic agents.

DOSAGE FORM, COMPOSITION AND PACKAGING

The tablets are white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel on one side and engraved “E435” on the other side, odorless.

1 tab. metoprolol tartrate 25 mg

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, colloidal anhydrous silicon dioxide, povidone, magnesium stearate.

30 pcs. - dark glass jars (1) - cardboard packs. 60 pcs. - dark glass jars (1) - cardboard packs.

PHARMACOLOGICAL ACTION

A cardioselective β-adrenergic receptor blocker that does not have intrinsic sympathomimetic and membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.

By blocking β1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular Ca2+ current, has a negative chrono-, dromo-, bathmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility).

At the beginning of the drug's use (in the first 24 hours after oral administration), the peripheral vascular resistance increases, after 1-3 days of use it returns to the initial level, and with further use it decreases.

The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin system and the central nervous system, restoration of the sensitivity of the baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, ultimately, a decrease in peripheral sympathetic influences. Reduces high blood pressure at rest, during physical exertion and stress.

Blood pressure decreases after 15 minutes, maximum after 2 hours; the effect lasts for 6 hours. A stable decrease is observed after several weeks of regular use.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic innervation. Reduces the frequency and severity of angina attacks and increases exercise tolerance.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions via the AV node) and along additional paths.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and hyperthyroidism, it reduces heart rate and can even lead to the restoration of sinus rhythm.

Prevents the development of migraine.

When taken for many years, it reduces cholesterol in the blood.

When used in average therapeutic doses, it has a less pronounced effect on organs containing β2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi, uterus) and on carbohydrate metabolism.

When used in high doses (more than 100 mg/day), it has a blocking effect on both subtypes of β-adrenergic receptors.

PHARMACOKINETICS

Suction

Quickly and completely (95%) absorbed from the gastrointestinal tract. Cmax in plasma is achieved 1.5-2 hours after oral administration. Bioavailability is 50%. During treatment, bioavailability increases to 70%. Eating increases bioavailability by 20-40%.

Distribution

Vd is 5.6 l/kg. Plasma protein binding - 12%. Penetrates the BBB and placental barrier. Excreted in breast milk in small quantities.

Metabolism

Metoprolol is biotransformed in the liver. Metabolites do not have pharmacological activity.

Removal

T1/2 averages 3.5-7 hours. Metoprolol is almost completely excreted in the urine within 72 hours. About 5% of the dose is excreted unchanged.

Pharmacokinetics in special clinical situations

With severe liver dysfunction, the bioavailability and T1/2 of metoprolol increases, which may require dose adjustment of the drug.

If renal function is impaired, T1/2 and systemic clearance of metoprolol do not change significantly.

INDICATIONS

Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs), incl. hyperkinetic type;

IHD (secondary prevention of myocardial infarction, prevention of angina attacks);

Heart rhythm disturbances (supraventricular arrhythmias, ventricular extrasystole);

Hyperthyroidism (as part of complex therapy);

Prevention of migraine attacks.

DOSING REGIME

For arterial hypertension, a daily dose of 50-100 mg/day is prescribed in 1 or 2 doses (morning and evening). If the therapeutic effect is insufficient, a gradual increase in the daily dose to 100-200 mg is possible.

For angina pectoris, supraventricular arrhythmias, for the prevention of migraine attacks, a dose of 100-200 mg/day is prescribed in 2 doses (morning and evening).

For secondary prevention of myocardial infarction, an average daily dose of 200 mg is prescribed in 2 divided doses (morning and evening).

For functional disorders of cardiac activity accompanied by tachycardia, a daily dose of 100 mg is prescribed in 2 divided doses (morning and evening).

In elderly patients, patients with impaired renal function, and also if hemodialysis is necessary, no change in dosage regimen is required.

In patients with severe liver dysfunction, the drug should be used in lower doses due to the slower metabolism of metoprolol.

The tablets should be taken orally during or immediately after meals. The tablets can be divided in half, but not chewed.

SIDE EFFECTS

From the central nervous system and peripheral nervous system: increased fatigue, weakness, headache, slower speed of mental and motor reactions; rarely - paresthesia in the limbs, depression, anxiety, decreased ability to concentrate, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, asthenic syndrome, muscle weakness.

From the senses: rarely - decreased vision, decreased secretion of tear fluid, xerophthalmos, conjunctivitis, tinnitus.

From the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension; rarely - decreased myocardial contractility, temporary worsening of symptoms of chronic heart failure, arrhythmias, increased peripheral circulatory disorders (coldness of the lower extremities, Raynaud's syndrome), myocardial conduction disorders; in isolated cases - AV block, cardialgia.

From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, dry mouth, change in taste; increased activity of liver transaminases; rarely - hyperbilirubinemia.

Dermatological reactions: urticaria, skin itching, rash, exacerbation of psoriasis, psoriasis-like skin changes, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when prescribed in high doses or in predisposed patients), shortness of breath.

From the endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia.

From the hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

Other: back or joint pain, slight weight gain, decreased libido and/or potency.

CONTRAINDICATIONS

Cardiogenic shock;

AV block II and III degrees;

Sinoatrial block;

Severe bradycardia (heart rate less than 50 beats/min);

Heart failure in the stage of decompensation;

Angiospastic angina (Prinzmetal's angina);

Severe arterial hypotension (systolic blood pressure below 100 mmHg);

Lactation period;

Concomitant use of MAO inhibitors;

Simultaneous intravenous administration of verapamil;

Hypersensitivity to metoprolol and other ingredients of the drug.

The drug should be prescribed with caution for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome), chronic liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, AV blockade of the first degree, thyrotoxicosis, depression (including a history), psoriasis, pregnancy, as well as children and adolescents under 18 years of age, elderly patients.

PREGNANCY AND LACTATION

The use of Egilok during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during this period, careful monitoring of the condition of the fetus and newborn is necessary for 48-72 hours after birth, since intrauterine growth retardation, bradycardia, arterial hypotension, respiratory depression, and hypoglycemia are possible.

The effect of metoprolol on a newborn during breastfeeding has not been studied, therefore women taking Egilok should stop breastfeeding.

SPECIAL INSTRUCTIONS

When prescribing Egilok, heart rate and blood pressure should be regularly monitored. The patient should be warned that if the heart rate is less than 50 beats/min, a doctor’s consultation is necessary.

In patients with diabetes mellitus, blood glucose levels should be regularly monitored and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

Prescribing Egilok to patients with chronic heart failure is possible only after reaching the compensation stage.

In patients taking Egilok, the severity of hypersensitivity reactions may increase (against the background of a burdened allergic history) and there may be no effect from the administration of usual doses of epinephrine (adrenaline).

The use of Egilok may worsen the symptoms of peripheral circulatory disorders.

Egilok should be discontinued gradually, gradually reducing its dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). During drug withdrawal, patients with angina pectoris should be under close medical supervision.

For exertional angina, the selected dose of the drug should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min.

Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid.

Metoprolol may mask some clinical manifestations of hyperthyroidism (tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.

In case of diabetes mellitus, taking Egilok can mask the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When prescribing metoprolol to patients with bronchial asthma, simultaneous use of beta2-adrenergic agonists is necessary.

In patients with pheochromocytoma, Egilok should be used in combination with alpha-blockers.

Before performing any surgical intervention, it is necessary to inform the anesthesiologist about the therapy being carried out with Egilok (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.

When prescribing the drug to elderly patients, liver function should be regularly monitored. Correction of the dosage regimen is required only if increasing bradycardia, a pronounced decrease in blood pressure, AV blockade, bronchospasm, ventricular arrhythmias, and severe liver dysfunction appear in elderly patients. Sometimes it is necessary to stop treatment.

Special monitoring should be carried out in patients with a history of depressive disorders. If depression develops, Egilok should be discontinued.

When using Egilok with clonidine simultaneously, if Egilok is discontinued, clonidine should be discontinued after a few days (due to the risk of withdrawal syndrome).

Drugs that reduce catecholamine levels (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.

Use in pediatrics

The effectiveness and safety of Egilok in children and adolescents under 18 years of age have not been determined.

Impact on the ability to drive vehicles and operate machinery

In patients whose activities require increased attention, the question of prescribing the drug on an outpatient basis should be decided only after assessing the patient’s individual response.

OVERDOSE

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arterial hypotension, arrhythmia, ventricular extrasystole, bronchospasm, fainting; in case of acute overdose - cardiogenic shock, loss of consciousness, coma, AV blockade up to the development of complete transverse block and cardiac arrest, cardialgia.

The first signs of overdose appear 20 minutes to 2 hours after administration.

Treatment: gastric lavage, prescription of adsorbents, symptomatic therapy: with a pronounced decrease in blood pressure - Trendelenburg position, in case of acute arterial hypotension, bradycardia and impending heart failure - intravenous (with an interval of 2-5 minutes) administration of beta-adrenergic stimulants or i.v. administration of 0.5-2 mg of atropine sulfate, in the absence of a positive effect - dopamine, dobutamine or norepinephrine. As subsequent measures, it is possible to prescribe 1-10 mg of glucagon and install a transvenous intracardial pacemaker. For bronchospasm - intravenous administration of beta2-adrenergic stimulants, for convulsions - slow intravenous administration of diazepam. Metoprolol is poorly excreted by hemodialysis.

DRUG INTERACTIONS

With simultaneous use of Egilok with MAO inhibitors, a significant increase in the hypotensive effect is possible. The break between taking MAO inhibitors and Egilok should be at least 14 days.

Simultaneous intravenous administration of verapamil can provoke cardiac arrest; simultaneous administration of nifedipine leads to a significant decrease in blood pressure.

Inhalation anesthetics (hydrocarbon derivatives) when used simultaneously with Egilok increase the risk of inhibition of myocardial contractile function and the development of arterial hypotension.

When used simultaneously, beta-agonists, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduce the hypotensive effect of Egilok.

With the simultaneous use of Egilok and ethanol, an increased inhibitory effect on the central nervous system is observed.

With simultaneous use of Egilok with ergot alkaloids, the risk of peripheral circulatory disorders increases.

When used simultaneously, Egilok increases the effect of oral hypoglycemic drugs and insulin and increases the risk of developing hypoglycemia.

When Egilok is used simultaneously with antihypertensive drugs, diuretics, nitrates, and calcium channel blockers, the risk of developing arterial hypotension increases.

With simultaneous use of Egilok with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, agents for general anesthesia and cardiac glycosides, an increase in the severity of the decrease in heart rate and inhibition of AV conduction may be observed.

Inducers of microsomal liver enzymes (rifampicin, barbiturates) accelerate the metabolism of metoprolol, which leads to a decrease in the concentration of metoprolol in the blood plasma and a decrease in the effect of Egilok.

Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in the blood plasma.

Allergens used for immunotherapy or allergen extracts for skin testing when used together with Egilok increase the risk of systemic allergic reactions or anaphylaxis.

Egilok, when used simultaneously, reduces the clearance of xanthines, especially in patients with initially increased clearance of theophylline under the influence of smoking.

When used simultaneously with Egilok, the clearance of lidocaine decreases and the concentration of lidocaine in plasma increases.

With simultaneous use, Egilok enhances and prolongs the effect of non-depolarizing muscle relaxants; prolongs the effect of indirect anticoagulants.

When used together with ethanol, the risk of a pronounced decrease in blood pressure increases.

CONDITIONS OF VACATION FROM PHARMACIES

The drug is available with a prescription.

CONDITIONS AND DURATION OF STORAGE

List B. The drug should be stored out of the reach of children at a temperature of 15° to 25°C. Shelf life - 5 years.

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Egilok: instructions for use, description and action

The drug Egilok (instructions for use will be presented below) is a heart blocker. With the help of these medical tablets, you can quickly and effectively reduce high blood pressure, eliminate heart pain and disruptions in the general functioning of the myocardium. Also, the drug can improve the general well-being of the patient, so it is often prescribed by cardiologists for acute and chronic heart failure.

In addition, Egilok (instructions for use are provided by the pharmacological manufacturer) has a pronounced antiarrhythmic therapeutic effect. It is able to normalize heart function and stabilize the frequency of myocardial muscle contractions. The drug also acts as a prophylactic against migraine.

With the correct dosage, Egilok (the instructions for use are quite clear and accessible to everyone) begins to exert its therapeutic effect just an hour and a half after the initial dose. Thus, the drug is absorbed quite quickly into the digestive system and begins to act.

The medicine is excreted in the urine. It is also absorbed in the patient's liver. For this reason, patients with liver dysfunction (hepatitis, etc.) sometimes require a slight dose adjustment. Moreover, in this state, people should be extremely careful to prevent an overdose.

In any form of release and dosage, Egilok has a pronounced hypotensive and antiarrhythmic effect. Due to this, it is able to favorably influence the functioning of the myocardial ventricles and the general functioning of the heart muscle.

With regular treatment with this drug, the patient's risk of death from heart attack and stroke is reduced. The overall load on the heart also decreases and its oxygen supply improves.

Due to this, the heart works more smoothly, without sudden failures and disturbances. This, in turn, acts as a prevention of angina pectoris, arrhythmia, tachycardia and other dangerous diseases.

It is also worth noting that treatment with Egilok reduces the likelihood of recurrent myocardial infarction, so it is indicated for people with this diagnosis.

Moreover, with a full course of treatment with this medicine, a person’s physical endurance increases, which is why he can put more emotional and sports stress on his body, without harm to health.

About how long you can take Egilok without a break, and for whom it is contraindicated, read further in the article.

Before considering the drug Egilok, for which it is prescribed, it is worth mentioning the form of release of this drug.

Egilok (indications for use can be quite different) is available in the form of white tablets. They do not have a characteristic odor. Each such tablet has a distinctive inscription “E435”.

Today, this drug has a fairly wide therapeutic focus. Despite this, not everyone knows who Egilok is indicated for and why it is prescribed. Egilok has an undeniable healing effect.

The following conditions and diseases are distinguished for which Egilok is prescribed (indications for use):

1. Severe arterial hypertension in men and women of different age categories.
2. Comprehensive treatment of migraine, as well as prevention of its development.
3. Acute angina, tachycardia or arrhythmia, as well as general cardiac arrhythmia.
4. Prevention of secondary development of myocardial infarction, when the patient is at risk of disease progression.
5. General disturbance of heart contractions (supraventricular pathologies).

Egilok, the indications for use of which were discussed above, also has a number of contraindications, that is, conditions in which this drug can be harmful to a person or even dangerous to his health.

The main contraindications to prescribing this drug to a patient are:

1. The patient's childhood (up to eighteen years). The drug is not prescribed for children. If necessary, the attending physician should look for a more suitable replacement.
2. Bradycardia.
3. Bronchial asthma in severe form.
4. Shock (cardiogenic form).
5. Individual intolerance by the patient to the active or auxiliary substances of the drug.
6. Advanced form of asthma.

Egilok is prescribed with caution for patients with diabetes mellitus, acute or chronic liver failure, as well as during pregnancy (when the benefits for the woman are higher than the possible risks for the fetus).

It is important to note that therapy with this drug must be carried out in a hospital setting under close medical supervision. This is especially true for the treatment of patients with severe chronic diseases, as well as during acute pathologies.

For the effect of treatment to be noticeable, you need to learn how to take Egilok correctly.

Before we look at how to take Egilok, it should be said that elderly patients do not need to adjust the dosage of the drug.

So how to take Egilok? These tablets should be taken after meals and washed down with a small amount of still water.

The dosage of the medicine and the duration of treatment are selected by the attending physician on an individual basis.

The permissible daily dosage is 200 mg.

• For migraine and for its prevention, you need to take two tablets twice a day.
• For arterial hypertension, you need to take 50 mg twice a day.
• For the treatment of angina pectoris, 50 mg of the drug is prescribed three times a day.
• After a heart attack, you need to take 200 mg per day. Divide the dose into two doses.
• If there is a history of arrhythmia or other diseases, Egilok is still not prescribed to children. This drug should not be prescribed to patients under eighteen years of age.

Not everyone knows how to take Egilok during pregnancy and whether it can be done at all. In fact, taking Egilok during pregnancy and breastfeeding (lactation) is highly discouraged by doctors.

Despite this, Egilok is sometimes used during pregnancy, but only when the benefit to the woman is higher than the expected risks to the fetus.

There is an increased risk of taking Egilok during pregnancy in the first trimester, when the foundations of the future organism and its systems are being laid.

When taking the drug in the last trimester of pregnancy, treatment should be stopped two days before delivery. Monitoring of the condition of the woman and newborn child is also necessary for another week.

If it is necessary to prescribe this medication while breastfeeding, the woman should stop breastfeeding and transfer the child to artificial feeding with formula.

To avoid severe allergic reactions, if the patient is hypersensitive, you should carefully combine Egilok with other drugs.

Thus, Egilok should be combined with caution with other antiarrhythmic drugs, as well as drugs to lower blood pressure.

Be sure to adjust the dose of Egilok when prescribing it simultaneously with Diclofenac, Theophylline and Reserpine.

Egilok, whose side effects are quite rare, is usually well tolerated by patients.

The drug Egilok (contraindications should not be violated, so as not to provoke undesirable consequences), most often causes the following adverse reactions in the body:

1. The most common disorders in the central nervous system are headaches, weakness, fatigue and sleep disturbances. Less common are depressive states, seizures, impaired attention and nervous agitation.
2. On the part of the heart, myocardial blockade, disturbances in heart rhythm and bradycardia may develop. This usually develops with an overdose of the drug.
3. In the digestive system, patients may experience abdominal tenderness, diarrhea, taste disturbances, and nausea. Constipation and liver dysfunction are rare.

Egilok, whose side effects occur infrequently, in isolated cases can cause the following undesirable reactions in people:

1. Impotence.
2. Dry eyes.
3. Noises in the ears.
4. Visual impairment.
5. Rash.

If a larger dose of the drug is taken (overdose), a person may experience a sharp decrease in blood pressure, vomiting, nausea and heart failure. In more severe cases, there is coma, shock and asystole.

Treatment of an overdose of this medicine is carried out based on the observed symptoms. In any case, primary therapy is aimed at stabilizing the general condition of the patient. Further therapy is aimed at eliminating malfunctions in the body.

Egilok, which contains contraindications in the instructions for use, has several effective analogues, that is, drugs with an identical therapeutic focus. Thus, instead of Egilok, the attending physician may prescribe Betelok, Metocard and Metoprolol. Metocard and Corvitol are used less frequently.

You can buy Egilok (its side effects are also described in the instructions) at almost any pharmacy. On average, its cost is 150 rubles per package of tablets.

It is important to remember that you can take this drug only after a doctor’s prescription. Self-therapy can be harmful to health.

To better understand the effect of treatment with Egilok, here are reviews from those patients who have already tried it on themselves:

1. Elena “I have been suffering from heart failure for a long time. The last time I was admitted to the hospital with a suspicion of myocardial infarction, but, fortunately, it was not confirmed. To normalize my condition, the attending physician prescribed me the drug Egilok. After a month of taking it, I began to feel much better. Heart pain and irregularities in heart rhythm disappeared. This medicine personally helped me a lot.”
2. Daniil “I suffered two myocardial infarctions. I tried many different drugs and the last one was Egilok. It improved my condition, but at the same time caused headaches and abdominal discomfort. The feeling is twofold."
3. Mikhail “I have diabetes and frequent attacks of arterial hypertension. The attending doctor prescribed me Egilok to normalize my blood pressure and eliminate headaches. I've been taking the drug for two weeks now. “The general condition is good, there are no side effects.”

med88.ru

Egilok

Egilok is considered a very effective remedy that has a positive effect on the functioning of the cardiovascular system. This drug reduces the heart rate and is also effective in stopping ventricular extrasystoles and atrial fibrillation. The main component of the drug Egilok is metoprolol, which belongs to the group of selective adrenergic blockers.

Egilok - what it helps with

Egilok is used for heart problems, as it belongs to the group of cardioselective beta-blockers. Thanks to the action of metoprolol, which is its main component, blood pressure levels are reduced, symptoms of arrhythmia and manifestations of angina are eliminated.

The effect of the drug is prolonged because it produces its effect by reducing peripheral vascular resistance gradually and moderately. In the case of left ventricular myocardial hypertrophy, which very often occurs in hypertensive patients, Egilok reduces the mass of the previously enlarged myocardium. It should also be noted that it has the ability to reduce myocardial oxygen demand.

As for the indications for the use of this remedy, these include:

• Attacks of migraine pain;
• Increased blood pressure levels;
• Presence of compensated heart failure;
• Manifestations of angina and other clinical symptoms of coronary heart disease;
• Pathological changes in heart rhythm, which include supraventricular tachycardia, as well as a decrease in heart rate due to atrial fibrillation or the occurrence of extrasystoles).

Egilok is also used as part of complex therapy for myocardial infarction.

Contraindications for use

Taking this medication is contraindicated in the following situations:

• Pregnancy and lactation period;
• Prinzmital's angina;
• Atrioventricular block of 2 and 3 degrees;
• Significant decrease in heart rate;
• Hypersensitivity to the components of this drug, which may cause an allergic reaction;
• Decompensated heart failure;
• Blockade of nerve impulses through the sinoatrial node;
• Cardiogenic and other types of shock;
• Significant reduction in blood pressure.

How and how much to take egilok

This medicine can be taken orally regardless of the time of day or meal. The individual dosage should be selected carefully, starting with the minimum amount of Egilok. The maximum daily dose is 200 milligrams. To achieve maximum effect, you should take the medicine regularly, since in this case a cumulative scheme operates. To reduce blood pressure, you need to start by taking 25 milligrams twice a day, after which, if necessary, the dose is gradually increased.

While taking Egilok, you should try to maintain your heart rate at 60 per minute, and after exercise it is advisable that it does not exceed 110 per minute.

In cases of migraine, as well as during the rehabilitation period after myocardial infarction, this drug is taken one hundred milligrams per day, dividing the dose into two doses, morning and evening.

Side effects

Side effects include:

• Shortness of breath, bronchospasm;
• Nausea, bradycardia, hypotension;
• Headache, epigastric pain;
• Allergy.

Egilok and alcohol

It has been noted by many studies that when interacting with ethyl alcohol, Egilok significantly inhibits the functioning of the central nervous system.

otchego.net

Egilok

Egilok is a beta-blocker used in the treatment of arterial hypertension and cardiac arrhythmias.

Release form and composition of Egilok

The drug is available in the form of white tablets, the main active ingredient of which is metoprolol tartrate.

The following excipients are used in Egilok tablets: sodium carboxymethyl starch, microcrystalline cellulose, anhydrous colloidal silicon dioxide, magnesium stearate, povidone.

Egilok is available in tablets of 25, 50 and 100 mg.

Pharmacological action of Egilok

Egilok is a cardioselective β-adrenergic receptor blocker that does not have membrane-stabilizing and sympathomimetic intrinsic activity.

The drug has antihypertensive, antiarrhythmic and antianginal effects.

The antihypertensive effect is based on a decrease in the synthesis and cardiac output of renin, inhibition of the activity of the central nervous and renin-angiotensin systems, and restoration of the sensitivity of the baroreceptors of the aortic arch. All this leads to a decrease in sympathetic peripheral influences.

The drug is able to reduce high blood pressure, both at rest and during stress and exercise.

A decrease in blood pressure occurs after 15 minutes, the effect of the drug lasts for 6 hours. A stable decrease in blood pressure occurs with regular use of the drug for several weeks.

The antiarrhythmic effect of Egilok is associated with the elimination of tachycardia, increased cAMP content, arterial hypertension, increased activity of the sympathetic nervous system, a decrease in the rate of spontaneous excitation of ectopic and sinus pacemakers, and a slowdown of AV conduction.

The antianginal effect is associated with a decrease in myocardial oxygen demand due to a decrease in heart rate and contractility, and a decrease in the sensitivity of the myocardium to sympathetic innervation. The drug helps improve exercise tolerance and reduce the frequency and severity of angina attacks.

Egilok prevents the development of migraine.

Indications for use of Egilok

According to the instructions, Egilok is used for:

• arterial hypertension, both in combination with other antihypertensive drugs and in monotherapy;
• heart rhythm disturbances;
• IHD as a means of preventing angina attacks and as secondary prevention of myocardial infarction;
• hyperthyroidism (in complex therapy);

and also as a prophylactic to prevent migraine attacks.

Contraindications to the use of Egilok

According to the instructions, Egilok is not used for:

• severe bradycardia;
• cardiogenic shock;
• SSSU;
• sinoatrial and AV blockades of the second and third degrees;
• hypersensitivity of the patient to metoprolol and other components of the drug;
• decompensation of heart failure;
• intravenous administration of verapamil;
• angiospastic angina;
• severe arterial hypotension;
• taking MAO inhibitors;
• lactation.

According to indications, Egilok is prescribed cautiously for:

• metabolic acidosis;
• intermittent claudication and Raynaud's syndrome;
• diabetes mellitus;
• bronchial asthma;
• chronic obstructive bronchitis;
• emphysema;
• chronic liver and kidney failure;
• thyrotoxicosis;
• myasthenia gravis;
• depression;
• pheochromocytoma;
• psoriasis;
• AV blockade of the first degree;
• pregnancy;

as well as elderly patients and children and adolescents under 18 years of age.

Method of application and dosage of Egilok

According to indications, Egilok tablets are taken orally after meals.

Daily dose of the drug:

• for arterial hypertension 50-100 mg, divided into 1-2 doses. It is possible to increase the dose if the effect of treatment is insufficient to 100-200 mg;
• for supraventricular arrhythmias, angina pectoris and for the prevention of migraine – 100-200 mg (2 doses);
• for functional disorders of cardiac activity with tachycardia – 100 mg (2 doses);
• for secondary prevention of myocardial infarction – 200 mg (2 doses).

In cases of severe liver dysfunction, the drug is prescribed in smaller dosages.

Side effects of Egilok

According to reviews, Egilok may cause side effects.

Cardiovascular system: palpitations, sinus bradycardia, decreased blood pressure, orthostatic hypotension.

Central and peripheral nervous systems: weakness, increased fatigue, slowed motor and mental reactions, headache.

Digestive system: abdominal pain, nausea, vomiting, constipation, diarrhea, change in taste, dry mouth, increased activity of liver enzymes.

Respiratory system: difficulty exhaling, nasal congestion, shortness of breath.

Hematopoietic system: agranulocytosis, thrombocytopenia, leukopenia.

Dermatological reactions: skin itching, urticaria, rash, psoriasis-like skin changes, exacerbation of psoriasis, exanthema, skin hyperemia, photodermatosis, alopecia, increased sweating.

Other: slight weight gain, joint and back pain, decreased libido.

Overdose

According to reviews of Egilok, an overdose of the drug is manifested by: nausea, vomiting, dizziness, severe sinus bradycardia, cyanosis, arterial hypotension, ventricular extrasystole, arrhythmia, bronchospasm, fainting.

Acute overdose is manifested by loss of consciousness, cardiogenic shock, cardialgia, coma, AV block, even cardiac arrest.

To treat an overdose, use: gastric lavage followed by the administration of adsorbents and symptomatic therapy.

Interaction with other drugs

When using Egilok according to indications simultaneously with:

• MAO inhibitors – the hypotensive effect is enhanced;
• verapamil can lead to cardiac arrest;
• nifedipine – significantly reduces blood pressure;
• beta-adrenergic stimulants, estrogens, theophylline, indomethacin, cocaine - the hypotensive effect is reduced;
• oral hypoglycemic insulin preparations – the risk of developing hypoglycemia increases;
• antihypertensive drugs, nitrates, diuretics, calcium channel blockers - the risk of arterial hypotension increases;
• verapamil, antiarrhythmic drugs, diltiazem, guanfacine, reserpine, clonidine, methyldopa, general anesthesia, cardiac glycosides - AV conduction is depressed and heart rate decreases;
• rifampicin and barbiturates - accelerates the metabolism of metoprolol;
• cimetidine, phenothiazines, oral contraceptives - the level of metoprolol in plasma increases;
• allergens – the risk of developing systemic allergic reactions and anaphylactic shock increases;

Egilok's analogues

Analogues of Egilok are Betalok, Vazocardin, Corvitol, Metocard, Lidalok, Metozok, Metolol, Metoprolol, Emzok.